Autotaxin structure–activity relationships revealed through lysophosphatidylcholine analogs

…, DA Osborne, PK Bridson, DL Baker, AL Parrill

Index: North, E. Jeffrey; Osborne, Daniel A.; Bridson, Peter K.; Baker, Daniel L.; Parrill, Abby L. Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 9 p. 3433 - 3442

Full Text: HTML

Citation Number: 25

Abstract

Autotaxin (ATX) catalyzes the hydrolysis of lysophosphatidylcholine (LPC) to form the bioactive lipid lysophosphatidic acid (LPA). LPA stimulates cell proliferation, cell survival, and cell migration and is involved in obesity, rheumatoid arthritis, neuropathic pain, atherosclerosis and various cancers, suggesting that ATX inhibitors have broad therapeutic potential. Product feedback inhibition of ATX by LPA has stimulated structure–activity ...